Cathepsin K Inhibitor

E-64 (Proteinase inhibitor E 64) is a potent irreversible inhibitor against general cysteine proteases with IC₅₀ of 9 nM for papain.

Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID₅₀ of 40 nM for Calpain I in human platelets. Calpeptin is also an inhibitor of cathepsin K.

Odanacatib (MK-0822) is a potent and selective inhibitor of cathepsin K, with an IC₅₀ of 0.2 nM for human cathepsin K.

MV061194 is a selective cathepsin K inhibitor with a human K_i of 2.5 nM. MV061194 can be used for the research of osteoporosis.

Balicatib (AAE581) is a potent, orally active and selective cathepsin K inhibitor with IC₅₀ values of 22, 61, 48, 2900 nM for cathepsin K, cathepsin B, cathepsin L, cathepsin S, respectively. Balicatib inhibits bone turnover, decreases bone formation rates. Balicatib has the potential for the research of osteoporosis.

LHVS is a potent, non-selective, irreversible, cell-permeable cysteine protease and cathepsin inhibitor. LHVS decreases actin ring formation. LHVS inhibits T. gondii invasion with an IC₅₀ of 10 μM.

Relacatib (SB-462795) is a novel, potent, and orally active inhibitor of human cathepsins K, L, and V with K_i values of 41 pM, 68 pM, and 53 pM, respectively. Relacatib inhibits endogenous cathepsin K in situ in human osteoclasts and human osteoclast-mediated bone resorption with IC₅₀ values of 45 nM and 70 nM, respectively. Relacatib inhibits bone resorption in vitro in human tissue as well as in cynomolgus monkeys in vivo.

L-006235 (L-235) is a potent, selective, reversible and orally active inhibitor of cathepsin K, with an IC₅₀ of 5 nM in bone resorption assay. L-006235 shows selectivity for cathepsin K (K_i=0.2 nM) over cathepsin B, cathepsin L, and cathepsin S (K_i=1, 6, and 47 μM, respectively). L-006235 can reduce collagen degradation and prevent bone loss.

VBY-825 is an orally available novel reversible cathepsin inhibitor that has high inhibitory potency against cathepsin B, L, S and V, and possesses anti-tumor, anti-inflammatory and analgesic effects.

3-Epiursolic Acid is a triterpenoid that can be isolated from Eriobotrya japonica, acts as a competitive inhibitor of cathepsin L (IC₅₀, 6.5 μM; K_i, 19.5 μM), with no obvious effect on cathepsin B.

2-Cyanopyrimidine is a potent and non-selective cysteine protease cathepsin K inhibitor with an IC₅₀ of 170 nM. 2-Cyanopyrimidine is used for osteoporos.

ONO-5334 is a potent, selective and orally active cathepsin K inhibitor with K_i values of 0.10 nM, 0.049 nM and 0.85 nM for human, rabbit and rat cathepsin K, respectively. ONO 5334 is an effective antiviral compound against SAR-COV-2 virus activity with an EC₅₀ value of 500 nM. ONO-5334 has the potential for the study of osteoporosis and COVID-19 disease.

Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a K_i of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen.

L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor, with IC₅₀s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively. L-873724 also exhibits an IC₅₀ of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption.

Cathepsin K inhibitor 6 (compound 19) is an inhibitor of cathepsin K (Cat K) with an IC₅₀ of 17 nM. Cathepsin K inhibitor 6 also has inhibitory effects on other isoforms, with IC₅₀s of 0.05 μM (Cat L) and 0.3 μM (Cat B), respectively.

Cathepsin K inhibitor 3 (compound 23) is a highly selective cathepsin K inhibitor with an IC₅₀ value of 0.5 nM. Cathepsin K inhibitor 3 has a favorable pharmacokinetic profile and may be used in osteoarthritis (OA) disease studies.

ABP 25 is an activity-based probe for cathepsin K imaging with excellent potency and selectivity.

Cathepsin K-IN-9 is a selective, potent and orally active Cathepsin K inhibitor with an IC₅₀ of 6.2 nM. Cathepsin K-IN-9 has IC₅₀ > 10000 nM for cathepsin B, L, and S, showing over 1600-fold selectivity. Cathepsin K-IN-9 has excellent safety and metabolic stability.Cathepsin K-IN-9 can be used for the research of osteoporosis.

SARS-CoV-2 3CLpro-IN-34 (Compound 55) is a highly efficient non-covalent inhibitor of the SARS-CoV-2 3CL^pro protease (b. SARS-CoV-2 3CL^pro protease) with an IC₅₀ of 1.9 μM. SARS-CoV-2 3CLpro-IN-34 can inhibit the 3CL^pro protein of SARS-CoV-1, with its IC₅₀ being 3.2 μM, and it shows high selectivity towards host cysteine proteases (such as cathepsins L/K and calpain). SARS-CoV-2 3CLpro-IN-34 exhibits antiviral activity in cells infected with SARS-CoV-2, with its EC₅₀ being 25 μM, and it is not affected by P-gp inhibitors and shows no significant cytotoxicity. SARS-CoV-2 3CLpro-IN-34 can be used for research on SARS-CoV-2 infection.